A cell-permeable triaminopyrimidine that selectively and reversibly blocks Cdk4/cyclin D1 and Cdk6/cyclin D1 activity (IC50s = 1.5 and 5.6 μM

Cdk4/6 Inhibitor IV – 1 mg

Brand:
Cayman
CAS:
359886-84-3
Storage:
-20
UN-No:
Non-Hazardous - /

Cdk4/6 inhibitor IV is a cell-permeable triaminopyrimidine that reversibly blocks Cdk4/cyclin D1 and Cdk6/cyclin D1 activity with IC50 values of 1.5 and 5.6 μM, respectively.{29264} It demonstrates potent selectivity for Cdk4/6 over Cdk5/p35, v-abl, c-met, IGF-1R, insulin receptor, Cdk2/cyclin A, Cdk2/cyclin E, Cdk4/cyclin D2, Cdk6/cyclin D2, and Cdk1/cyclin B (IC50s = > 10-100 µM).{29264} At 5-10 µM, this compound blocks retinoblastoma protein phosphorylation at Ser780 and Ser795, inducing cell cycle arrest in the G1 phase and apoptosis in asynchronous cell lines.{29264} In mice bearing human HCT116 colon carcinoma xenografts, 30 mg/kg, i.p. Cdk/6 inhibitor IV suppressed tumor growth after 29 days of treatment.{29264}  

 

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Description

A cell-permeable triaminopyrimidine that selectively and reversibly blocks Cdk4/cyclin D1 and Cdk6/cyclin D1 activity (IC50s = 1.5 and 5.6 μM, respectively); induces cell cycle arrest in the G1 phase and apoptosis in asynchronous cell lines; suppresses tumor growth in mice bearing human HCT116 colon carcinoma xenografts

Formal name: trans-4-[[6-(ethylamino)-2-[[1-(phenylmethyl)-1H-indol-5-yl]amino]-4-pyrimidinyl]amino]-cyclohexanol

Synonyms:  CINK4|Cyclin-dependent kinase 4/6 Inhibitor IV

Molecular weight: 456.6

CAS: 359886-84-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|CDKs||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle|G1||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling

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